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Dacomitinib [1110813-31-4]

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Referência HY-13272-50mg

Tamanho : 50mg

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Marca : MedChemExpress

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Description

Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively^[1].

IC₅₀ & Target^[1]

EGFR

6 nM (IC₅₀)

ErbB2

45.7 nM (IC₅₀)

ErbB4

73.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	GI₅₀	6 nM Compound: 2	Antiproliferative activity against human A-431 cells harboring EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay Antiproliferative activity against human A-431 cells harboring EGFR assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay	[PMID: 37499291]
A-431	IC₅₀	1.96 μM Compound: Dacomitinib	Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
A549	IC₅₀	>10 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human A549 cells harboring K-ras G12S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human A549 cells harboring K-ras G12S mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
A549	IC₅₀	0.49 μM Compound: Dacomitinib	Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells harboring EGFR wild type assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
BaF3	IC₅₀	<1 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.2 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR vIII mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.4 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.6 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	1.9 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	140 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_A750/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	160 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_P753InsS/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	2 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	2.6 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	230 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR A767_V769duspASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR A767_V769duspASV mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	240 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del L747_A750InsP/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	270 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del E746_S752InsV/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	300 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BaF3	IC₅₀	330 nM Compound: Chemical probe: PF-00299804	Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR Del S752_I759/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
BT-474	IC₅₀	18 nM Compound: Dacomitinib	Antiproliferative activity against human BT-474 cells Antiproliferative activity against human BT-474 cells	[PMID: 33429247]
Calu-3	IC₅₀	0.063 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human Calu-3 cells overexpressing ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human Calu-3 cells overexpressing ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
H322	IC₅₀	>10 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human H322 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human H322 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC4006	IC₅₀	0.004 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC4006 cells harboring EGFR Del L747_E749 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC4006 cells harboring EGFR Del L747_E749 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	GI₅₀	5 nM Compound: 2	Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay Antiproliferative activity against human HCC827 cells harboring EGFR del19 mutant assessed as cell growth inhibition incubated for 72 hrs by Celltiter Glo assay	[PMID: 37499291]
HCC827	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.003 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.007 μM Compound: Dacomitinib	Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
HCC827	IC₅₀	0.014 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.061 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HCC827	IC₅₀	0.083 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 Ins 774YVMA assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR Del E746_A750 mutant transfected with ERBB2 Ins 774YVMA assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
HEK293	IC₅₀	0.185 μM Compound: Dacomitinib	Cytotoxicity against HEK293 cells expressing ABCG2 in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2 in presence of methotrexate	[PMID: 35944339]
LoVo	IC₅₀	0.011 μM Compound: 5	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	GI₅₀	123.3 nM Compound: Dacomitinib	Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition	[PMID: 26310890]
NCI-H1975	IC₅₀	0.042 μM Compound: 5	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	IC₅₀	0.042 μM Compound: 5	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	IC₅₀	0.44 μM Compound: 32; PF00299804	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay	[PMID: 28754471]
NCI-H1975	IC₅₀	0.44 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H1975	IC₅₀	0.7 μM Compound: Dacomitinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell growth incubated for 48 to 72 hrs by CCK-8 assay	[PMID: 38759458]
NCI-H3255	IC₅₀	0.007 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	0.007 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with GFP assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	0.137 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR WT/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	1.57 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR Del L747_S752,P753S/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H3255	IC₅₀	1.62 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant transfected with EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
NCI-H441	IC₅₀	4 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human NCI-H441 cells harboring K-ras G12V mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H441 cells harboring K-ras G12V mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
PC-9	IC₅₀	0.00063 μM Compound: 5	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
PC-9	IC₅₀	0.002 μM Compound: Chemical probe: PF-00299804	Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay Antiproliferative activity against human PC-9 cells harboring EGFR Del E746_A750 mutant assessed as inhibition of cell growth incubated for 72 hrs by MTS assay	[PMID: 18089823]
PC-9	IC₅₀	0.63 nM Compound: 5	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
Sf9	IC₅₀	0.006 μM Compound: 54; PF-00299804	Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB1 (unknown origin) (Met-668 to Ala-1211 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	0.046 μM Compound: 54; PF-00299804	Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB2 (unknown origin) (Ile-675 to Val-1256 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	0.074 μM Compound: 54; PF-00299804	Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA Irreversible inhibition of GST-tagged ERBB4 (unknown origin) (Gly-259 to Gly-690 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in Glu/Tyr copolymer phosphorylation after 6 mins by ELISA	[PMID: 27491023]
Sf9	IC₅₀	3.57 μM Compound: 54; PF-00299804	Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA Irreversible inhibition of human recombinant GST-tagged JAK3 expressed in baculovirus infected Sf9 insect cells assessed as reduction in polyglutamic acid-tyrosine phosphorylation after 30 mins by ELISA	[PMID: 27491023]
SK-BR-3	IC₅₀	15 nM Compound: Dacomitinib	Antiproliferative activity against human SK-BR-3 cells Antiproliferative activity against human SK-BR-3 cells	[PMID: 33429247]

In Vitro

Dacomitinib (PF00299804) effectively inhibits the in vitro kinase activity of wild-type EGFR (IC50=6 nM)with similar efficacy. Dacomitinib also effectively inhibits wild-type ERBB2 with IC₅₀ of 45.7 nM. In H441, an IC₅₀ is reached with Dacomitinib but only at a very high concentration (4 μM) and likely reflects off-target effects. In cell lines wild-type for both EGFR and K-ras (H322, H1819, and Calu-3), ZD1839 and Dacomitinib both effectively inhibit growth of H1819 and Calu-3 cells but not of H322 cells. Dacomitinib is a pan-ERBB inhibitor and most EGFR mutant cell lines express multiple ERBB family members, the effects on EGFR phosphorylation could potentially be indirect. Dacomitinib inhibits EGFR phosphorylation in all of the different EGFR T790M proteins whereas ZD1839 is ineffective even at 10 μM. In the NIH3T3 cells, phosphorylation of EGFR L858R/T790M is completely inhibited by 1 nM Dacomitinib, whereas 100 nM or greater is required to inhibit EGFR WT/T790M or Del/T790M^[1]. The HER2-amplified cell lines are most sensitive to growth inhibition by Dacomitinib (IC₅₀<1 μM in 14 of 16 lines; 87.5%) as compared with 5 of 28 (17.9%) of HER2-nonamplified lines (excluding immortalized lines)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : 38.89 mg/mL (82.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1279 mL	10.6397 mL	21.2793 mL
5 mM	0.4256 mL	2.1279 mL	4.2559 mL
10 mM	0.2128 mL	1.0640 mL	2.1279 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.32 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC/saline water
Solubility: 5 mg/mL (10.64 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.74%

Fiche technique (282 KB) SDS (393 KB)

COA (252 KB) RP-HPLC (246 KB) MS (70 KB) Elemental Analysis Report (110 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67(24):11924-32. [Content Brief]

[2]. Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11(9):1978-87. [Content Brief]

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